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编 号：F627898
分子式：C26H21ClF3N3O5S
分子量：579.98
分子式：C26H21ClF3N3O5S
分子量：579.98
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CAS No: 1049704-18-8
产品详情
生物活性：
MA242 is a specific dual inhibitor of MDM2 and NFAT1. MA242 directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 induces apoptosis in pancreatic cancer cell lines regardless of p53 status.
体内研究：
MA242 (IP; 2.5, 5, 10 mg/kg) suppresses orthotopic pancreatic tumor growth in vivo, independent of p53. There were no significant differences in the average body weights between the vehicle- and MA242-treated mice in either of the models, did not have significant host toxicity at these effective doses.Animal Model:Female 4-6-week-old athymic nude mice (nu/nu, 4-6 weeks) bearing AsPC-1-Luc or Panc-1-Luc tumor
Dosage:2.5 or 5 mg/kg for Panc-1 tumor-bearing mice; 10 mg/kg for AsPC-1 tumor-bearing mice
Administration:IP; 2.5 or 5 mg/kg/d, 5 d/wk for five weeks for Panc-1 tumor-bearing mice;IP; 10 mg/kg/d, 5 d/wk for three weeks for AsPC-1 tumor-bearing mice
Result:Resulted in 56.1% and 82.5% inhibition of tumor growth in nude mice bearing Panc-1 orthotopic tumors, respectively. Significantly suppressed the growth of AsPC-1 orthotopic tumors by 89.5% (P < 0.01) compared with the tumors in control animals. Led to almost complete tumor regression in MD242-treated mice in both models.
体外研究：
MA242 (0.05-5 μM; 72 hours) significantly inhibits pancreatic cancer cell growth, with IC50s ranging from 0.1 to 0.4 μM, regardless of the p53 status of the cells. However, MA242 shows minimal effects on the growth of normal HPDE cells (IC50=5.81 μM), indicating that MA242 has selective effects against cancer cells. MA242 (0.1-0.5 μM; 24 hours) significantly decreases the MDM2 and NFAT1 protein levels at a low concentration in all three cell lines.MA242 decreases cell proliferation and induces apoptosis in pancreatic cancer cell lines regardless of p53 status. MA242 alone or in combination with Gemcitabine inhibits pancreatic tumor growth and metastasis without any host toxicity. MA242 exerts cytotoxicity against hepatocellular carcinoma (HCC) cells by inhibiting the NFAT1-MDM2 pathway in vitro, independent of p53. MA242 shows selective cytotoxicity against HCC cells, with IC50 values ranging from 0.1-0.31 μM.
MA242 is a specific dual inhibitor of MDM2 and NFAT1. MA242 directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 induces apoptosis in pancreatic cancer cell lines regardless of p53 status.
体内研究：
MA242 (IP; 2.5, 5, 10 mg/kg) suppresses orthotopic pancreatic tumor growth in vivo, independent of p53. There were no significant differences in the average body weights between the vehicle- and MA242-treated mice in either of the models, did not have significant host toxicity at these effective doses.Animal Model:Female 4-6-week-old athymic nude mice (nu/nu, 4-6 weeks) bearing AsPC-1-Luc or Panc-1-Luc tumor
Dosage:2.5 or 5 mg/kg for Panc-1 tumor-bearing mice; 10 mg/kg for AsPC-1 tumor-bearing mice
Administration:IP; 2.5 or 5 mg/kg/d, 5 d/wk for five weeks for Panc-1 tumor-bearing mice;IP; 10 mg/kg/d, 5 d/wk for three weeks for AsPC-1 tumor-bearing mice
Result:Resulted in 56.1% and 82.5% inhibition of tumor growth in nude mice bearing Panc-1 orthotopic tumors, respectively. Significantly suppressed the growth of AsPC-1 orthotopic tumors by 89.5% (P < 0.01) compared with the tumors in control animals. Led to almost complete tumor regression in MD242-treated mice in both models.
体外研究：
MA242 (0.05-5 μM; 72 hours) significantly inhibits pancreatic cancer cell growth, with IC50s ranging from 0.1 to 0.4 μM, regardless of the p53 status of the cells. However, MA242 shows minimal effects on the growth of normal HPDE cells (IC50=5.81 μM), indicating that MA242 has selective effects against cancer cells. MA242 (0.1-0.5 μM; 24 hours) significantly decreases the MDM2 and NFAT1 protein levels at a low concentration in all three cell lines.MA242 decreases cell proliferation and induces apoptosis in pancreatic cancer cell lines regardless of p53 status. MA242 alone or in combination with Gemcitabine inhibits pancreatic tumor growth and metastasis without any host toxicity. MA242 exerts cytotoxicity against hepatocellular carcinoma (HCC) cells by inhibiting the NFAT1-MDM2 pathway in vitro, independent of p53. MA242 shows selective cytotoxicity against HCC cells, with IC50 values ranging from 0.1-0.31 μM.
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